Anti-Ischemia Drugs Flashcards
What are the main determinants of oxygen supply to heart?
How are they impaired?
How is this fixed?
- Blood flow
- O2 carrying capacity of blood
Impaired by…
- Dec coronary perfusion pressure, inc coronary resistance, inc extrinsic compressive forces
- emphysema, pneumonia, change in altitude (less O2 supply)
- anemia or sickle cell (change Hb content)
Fix by…
- Inc oxygen supply, inc hematocrit
- Vasodilate coronary arteries
- Maintain BP to maintain coronary perfusion pressure
What are the main determinants of oxygen demand of heart?
How are these increased?
How is this fixed?
- Inc HR
- Inc Contractility
- Inc wall stress (greater P or V)
Increased if…
- adrenergics/symp NS
- anything that inc preload (vol) or after load (pressure)
Fix by…
- Dec HR
- Dec Ca++ influx
- Dec preload
- Dec afterload
Exogenous Nitrates in General (mechanism, types & dose dependence)
- MAO - converted to NO by mitochondrial aldehyde dehydrogenase
- Depends on dose
- @ low dose… venous dilation
- @ high dose … coronary artery dilation
- Short acting - mucosal (sublingual or oral spray) or transdermal (ointment) —> dir to blood so rapid onset that can be used for angina as needed; can also use prophylactically b/f activities that trigger angina
- Long acting - oral or sustained release patch
Positive Oxygen Effects of Nitrates
Dec coronary resistance, dec R3 b/c less preload, dec preload and after load so less wall tension (less demand)
5 Side Effects of Nitrates
- Nitrate tolerance (less potent over time); help by dosing so that they are nitrate free for 10-12 hrs a day (“”resensitization”)
- Headache/flushing - usually go away after 2 wks
- Hypotension - esp if on diuretic (DO NOT USE IF ALSO ON PDE INHIB - like Viagra)
- Hypoxemia - dilate vessels in hypoxic part of lung instead of oxygenated part of lung
- Tissue hypoxia if methemoglobinemia (rare)
What are the 2 long-acting nitrates? How do they differ?
- Isosorbide dinitrate - hepatic 1st pass —> isosorbide mononitrate
- Isosorbide mononitrate - already in active metabolite form so greater bioavailability; FASTER
3 Categories of Beta Blockers
- Cardioselective
- Intrinsic Sympathomimetics
- Alpha Receptor Blocking
Cardioselective Beta Blockers
- preferentially block beta 1 (however un-selective @ high doses)
- Atenolol, bisoprolol, betaxolol, esmolol, metoprolol
- Positive effects - dec HR and dec contractility so less demand; dec HR also allows more diastolic filling time so more coronary flow, some inc resistance
IAS Beta Blockers
- weak beta agonists that competitively inhibit the strong catecholamines from binding (shield from natural catecholamines)
- Pindolol, acebutolol, carteolol, penbutolol
- Do not use if CAD (may inc mortality)
- Pos effects - slight dec in HR and contractility but may inc after load - not used for CAD
Alpha Receptor Blocking Beta Blockers
- prevent unopposed alpha adrenergic stimulation during beta blockage so no compensatory vasoconstriction
- Labetolol, carvedilol
- Best for HTN
5 Side Effects of Beta Blockers
- CNS - esp if lipophilic (fatigue, sleep problems, depression, sexual dysfunction)
- Conduction abnormalities - dec SA node rate so brady
- CHF
- Exacerbate peropheral vascular disease
- Dec glycogen breakdown (normally sympathetic beta) so exacerbate DN hypoglycemia
Hydrophilic v. Lipophilic Beta Blockers
- Lipophilic = liver metabolism so shorter half-life & cross BBB so CNS side effects
- Hydrophilic = renal metabolism so longer half-life & do NOT cross BBB so less CNS effects
2 Categories of Ca Channel Blockers
- Dihydropyridines - more potent vasodilators
- Non - Dihydro (Benzothiazapines & Phenylalkylamines) - more potent effects on slowing SA and AV node - dec HR and conduction
Dihydropyridines
- Positive effects - dec coronary vascular resistance and dec R3 thru dilation, dec after load and preload by peripheral dilation so less wall tension
- Can induce reflex tachycardia
- Nifedipine, amlodipine, felodipine, nicardipine, isradipine
Non-dihydropyridines
- Positive effects - dec coronary resistance still thru vasodilation and dec HR and contractility so less demand
- Can result in symptomatic bradycardia or AV block (esp in verapamil so do not use w/ beta blocker for risk of complete block)
- Diltiazem & verapamil